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Design, synthesis, and evaluation of antitumor activity of quinazoline derivatives containing different terminal segments of basic amine groups

  • Shihao Wang,
  • Zichen Yang,
  • Dongling Gu,
  • JiaHui Han,
  • Hongjing Chen,
  • Hao Wang,
  • JiaXin Zheng,
  • Hongmin Liu,
  • Yu Ke,
  • Qiurong Zhang

摘要

In this study, we designed and synthesized 41 quinazoline derivatives with different base amine termini. Compound 15n showed the best antiproliferation activity against A549 cells with IC50 value of 1.91 μM in four cancer cell lines (MGC-803, PC-3, A549, and Eca-109). In colony, scratch, and apoptosis experiments, compound 15n inhibited proliferation, migration, and apoptosis of A549 cells in a concentration-dependent manner and blocked the cell cycle in the G0/G1 phase. Overall, our study suggests that compound 15n has potential as a lead compound for the development of antitumor drugs.